AI Article Synopsis
- The process involves cross-coupling these hydroxylamine benzoates with zinc chlorides to generate diverse polyfunctional tertiary amines.
- Notably, this synthesis was successfully applied to produce compounds like penfluridol and gepirone, which are pharmaceuticals.
Article Abstract
A general preparation of polyfunctional hydroxylamine benzoates from the corresponding secondary amines is reported. This convenient synthesis allows the setup of a late-stage functionalization of various secondary amines, including pharmaceuticals and peptidic derivatives. Thus, a cross-coupling of hydroxylamine benzoates with various alkyl-, aryl-, and heteroaryl-zinc chlorides in the presence of 5 mol % CoCl (25 °C, 2 h) provides a range of polyfunctional tertiary amines. This method was used to prepare penfluridol and gepirone.
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| http://dx.doi.org/10.1021/acs.orglett.8b03787 | DOI Listing |
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